| abstract |
In the compounds of the invention, R 1 is alkyl, alkenyl, alkynyl, aryl-Y 1, heteroaryl-Y 1 -, aryl (O) t-aryl-Y 1 -, aryl (O) t-heteroaryl-Y 1 -, heteroaryl. -aryl (O) t-aryl-Y1-, heteroaryl- (O) t-heteroaryl-Y1-, aryl-SO2-Y1-, alkyl-G-Y1-, heteroaryl-G-aryl-Y1-, J1- SO2-Y1-, R17O (CO-alkenyl-Y1-, R17NHCO-Y1-, R17NHSO2-Y1-, alkynyl-Y1-, alkenyl-Y1-, aryl-O-Y1-, heteroaryl-O-Y1-, alkyl- SO2-Y1, M-Y1, J1-Y1, J1-CO-Y1, aryl-CO-Y1 or cycloalkylY1 or cycloalkenyl-Y1, wherein the alkynyl and alkynyl-Y1 are optionally - Optionally substituted by one or more -COOR17, and optionally substituted by one or more hydroxy or alkyl groups, alkenyl optionally substituted with one or more -COOR17 groups, R2 being hydrogen or alkyl optionally substituted with R3; se is hydrogen or alkyl, or R1 and R2 together with the nitrogen atom to which they are attached are J2, wherein the nitrogen is X1 or X2, t is 0 or 1, X is ethylene or CReRf wherein Re and Rf are independently hydrogen or alkyl or Re and Rf R 4 and R 5 are independently hydrogen or alkyl, Z is a direct bond, CO, SO 2, CR 10 R 7 (CH 2) n, (CH 2) n CR 10 R 7, CHR 7 (CH 2) n O, CHR 7 (CH 2) n S, CHR 7 (CH 2); ) nOCO, CHR7 (CH2) nCO, COCHR7 (CH2) n or SO2CHR7 (CH2) n, R6 is alkyl, alkenyl, aryl, heteroaryl, arylalkenyl, cyano or -Y2-J3, R7 is hydrogen, alkyl, CONR8R9 or COO- (alkyl), a and b being 1 or 2, where a + b is 2 or 3, G is -SO2-, -SO2NR18-, -NR18SO2-, -NR18CO-, -CO- or-CONR18-, n is 0-4, M is cycloalkyl or cycloalkenyl fused to a monocyclic aryl group or a monocyclic heteroaryl group; sulfur, X2 is CH2, oxygen, NR12 or sulfur, m1 is 1-3, m2 is 1-3, with the constraint that h1 + m2 is 3-5, with the further limitation that when X1 and X2 are simultaneously oxygen, NR11, NR12 or sulfur, then m1 and m2 are at least 2, Y1, Y2 and Y3 are each independently a direct bond or - (CH2) pCRcRd (CH2) q-, wherein Rc and Rd are each independently hydrogen or alkyl or Rc and Rd are the carbon atom to which they are attached together cycloalkyl, p and q are independently 0-5, wherein p + q is 0-5. The present invention relates to the preparation of the above compounds |